Self-assembling hybrid linear-dendritic block copolymers: The design of nano-carriers for lipophilic antitumoral drugs

Two series of amphiphilic block copolymers with a hybrid linear-dendritic structure are presented. The compounds consisted of a hydrophilic poly (ethylene glycol) (PEG) block and a 2,2′-bis(hydroxymethyl)propionic acid (bis-MPA) dendron functionalized with stearic acid chains that impart a hydrophob...

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Detalles Bibliográficos
Autores: Fedeli, Elisabetta, Lancelot, Alexandre, Dominguez, Juan Manuel, Serrano, José Luis, Calvo, Pilar, Sierra, Teresa
Tipo de recurso: artículo
Estado:Versión publicada
Fecha de publicación:2019
País:España
Institución:Consejo Superior de Investigaciones Científicas (CSIC)
Repositorio:DIGITAL.CSIC. Repositorio Institucional del CSIC
OAI Identifier:oai:digital.csic.es:10261/177047
Acceso en línea:http://hdl.handle.net/10261/177047
Access Level:acceso abierto
Palabra clave:Dendrimers
Micellar aggregates
Drug delivery
Anticancer
Descripción
Sumario:Two series of amphiphilic block copolymers with a hybrid linear-dendritic structure are presented. The compounds consisted of a hydrophilic poly (ethylene glycol) (PEG) block and a 2,2′-bis(hydroxymethyl)propionic acid (bis-MPA) dendron functionalized with stearic acid chains that impart a hydrophobic nature to the block. Different self-assembled nanostructures with a hydrophobic interior and a hydrophilic external part were obtained depending on the length of the PEG chain (<i>M</i><sub>n</sub> = 2000 and <i>M</i><sub>n</sub> = 5000) and the generation of the bis-MPA dendron. The materials were characterized by transmission electron microscopy (TEM). The shapes of the aggregates ranged from spherical or cylindrical micelles to flexible bilayers. The hydrophobic core enabled these nanostructures to encapsulate the water-insoluble drug plitidepsin. The efficacy of these new plitidepsin-containing carriers was evaluated in four cancer cell-lines and they showed similar anticancer activity to the current standard drug formulation.